Geranyl dihydrochalcones from Artocarpus altilis and their antiausteric activity

Mai Thanh Thi Nguyen, Nhan Trung Nguyen, Khang Duy Huu Nguyen, Hien Thu Thi Dau, Hai Xuan Nguyen, Phu Hoang Dang, Tam Minh Le, Trong Huu Nguyen Phan, Anh Hai Tran, Bac Duy Nguyen, Jun Ya Ueda, Suresh Awale*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

32 Scopus citations

Abstract

Human pancreatic cancer cell lines have remarkable tolerance to nutrition starvation, which enables them to survive under a tumor microenvironment. The search for agents that preferentially inhibit the survival of cancer cells under low nutrient conditions is a novel antiausterity strategy in anticancer drug discovery. In this study, the methanolic extract of the leaves of Artocarpus altilis showed 100 % preferential cytotoxicity against PANC-1 human pancreatic cancer cells under nutrient-deprived conditions at a concentration of 50 μg/mL. Further investigation of this extract led to the isolation of eight new geranylated dihydrochalcones named sakenins A-H (1-8) together with four known compounds (9-12). Among them, sakenins F (6) and H (8) were identified as potent preferentially cytotoxic candidates with PC50 values of 8.0 μM and 11.1 μM, respectively.

Original languageEnglish
Pages (from-to)193-200
Number of pages8
JournalPlanta Medica
Volume80
Issue number2-3
DOIs
StatePublished - 2014/02

Keywords

  • Artocarpus altilis
  • Moraceae
  • PANC-1
  • antiausterity agent
  • pancreatic cancer

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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